Table 1.
Inhibition of Human Histone Methyltransferases by EPZ004777
| Enzyme | IC50 (nM)a | Fold Selectivityb |
|---|---|---|
| DOT1L | 0.4 ± 0.1 | 1.0 |
| CARM1 | >50,000 | >100,000 |
| EHMT2 | >50,000 | >100,000 |
| EZH1c | >50,000 | >100,000 |
| EZH2c | >50,000 | >100,000 |
| PRMT1 | >50,000 | >100,000 |
| PRMT5 | 521 ± 137 | 1280 |
| PRMT8 | >50,000 | >100,000 |
| SETD7 | >50,000 | >100,000 |
| WHSC1 | >50,000 | >100,000 |
a
IC50 is the concentration of compound resulting in 50% inhibition of enzyme activity. ± error represents the 95% confidence interval.
b
Fold selectivity is relative to DOT1L, and is calculated as the ratio of the IC50 for the enzyme under study over the IC50 for DOT1L.
c
Measured in the context of the PRC2 multiprotein complex.